Ahmed Nashaat Alnagar, Amira Motawea, Khaled M Elamin, Irhan Ibrahim Abu Hashim
{"title":"Hyaluronic acid/lactoferrin-coated polydatin/PLGA nanoparticles for active targeting of CD44 receptors in lung cancer.","authors":"Ahmed Nashaat Alnagar, Amira Motawea, Khaled M Elamin, Irhan Ibrahim Abu Hashim","doi":"10.1080/10837450.2024.2414937","DOIUrl":"10.1080/10837450.2024.2414937","url":null,"abstract":"<p><p>Traditional chemotherapeutic drugs lack optimal efficacy and invoke severe adverse effects in cancer patients. Polydatin (PD), a phytomedicine, has gradually gained attention due to its antitumor activity. However, its low solubility and poor bioavailability are still cornerstone issues. The present study aimed to fabricate and develop hyaluronic acid/lactoferrin-double coated PD/PLGA nanoparticles <i>via</i> a layer-by-layer self-assembly technique for active targeting of CD44 receptors in lung cancer. Different molecular weights (M.wt.) of HA (32 and 110 kDa) were exploited to study the relationship between the HA M.wt. and the NPs targeting efficacy. The optimized formulations were fully characterized. Their cytotoxicity and cellular uptake were investigated against A549 cell line by CCK-8 kit and fluorescence imaging, respectively. Finally, HA110/Lf-coated PD/PLGA NPs (F9) were subjected to a competitive inhibition study to prove internalization through CD44 overexpressed receptors. The results verified the fabrication of F9 with a particle size of 174.87 ± 3.97 nm and a zeta potential of -24.37 ± 1.19 mV as well as spherical NPs architecture. Importantly, it provoked enhanced cytotoxicity (IC<sub>50</sub> = 0.57 ± 0.02 µg/mL) and superior cellular uptake efficacy. To conclude, the current investigation lays the foundation for the prospective therapeutic avenue of F9 for active targeting of CD44 receptors in lung cancer.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1016-1032"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142400976","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Komlan Koumbogle, François Gitzhofer, Nicolas Abatzoglou
{"title":"Influence of punch coating surface properties on sticking during the tableting process.","authors":"Komlan Koumbogle, François Gitzhofer, Nicolas Abatzoglou","doi":"10.1080/10837450.2024.2413147","DOIUrl":"10.1080/10837450.2024.2413147","url":null,"abstract":"<p><strong>Introduction: </strong>The present study evaluates the sticking propensity of Uncoated steel, and chromium nitride (CrN), zirconium nitride (ZrN), titanium nitride (TiN) and Ultracoat punch coatings during the tableting process of microcrystalline cellulose (MCC) conducted on a Manesty<sup>®</sup> F3 single station tableting press.</p><p><strong>Methods: </strong>Surface properties including surface roughness, surface free energy (SFE) and its components, the atomic percentage of surface polar functional groups and oxides measured with X-ray photoelectron spectroscopy were used to characterize the surface propensity to sticking.</p><p><strong>Results: </strong>After five hours of tablet pressing, MCC powder particles were found to adhere to the TiN coated and the uncoated steel punches. Surface analysis show that surface roughness of all the tested punches was similar. The Lewis base SFE component (LB-comp) was found to govern the acid-base interactions of the tested surfaces, and its value was higher for punch surfaces affected by sticking. The surfaces exhibiting higher LB-comp are more prone to strong acid-base interactions with water molecules that evaporate from the powder bed during compression. Therefore, these surfaces adsorbed water and allow sticking through capillary adhesion force.</p><p><strong>Conclusion: </strong>The total atomic percentage of the surface polar functional groups (PFG) and oxides was also high for the surfaces that stick to MCC during tableting, suggesting that hydrophilic molecules on the punch surface favor sticking.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"987-995"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372523","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dong-Won Oh, Ji Hoon Choi, Gweon Hee Yu, Bo Kyung Kim, Sang Min Cho, Youn Woong Choi, Jin-Hyuk Jeong, Ji-Hyun Kang, Dong-Wook Kim, Chun-Woong Park
{"title":"Formulation and evaluation of carrier-based dry powders containing budesonide and arformoterol for inhalation therapy.","authors":"Dong-Won Oh, Ji Hoon Choi, Gweon Hee Yu, Bo Kyung Kim, Sang Min Cho, Youn Woong Choi, Jin-Hyuk Jeong, Ji-Hyun Kang, Dong-Wook Kim, Chun-Woong Park","doi":"10.1080/10837450.2024.2413145","DOIUrl":"10.1080/10837450.2024.2413145","url":null,"abstract":"<p><p>Asthma and Chronic Obstructive Pulmonary Disease (COPD) are major global health concerns, with inhalation therapy being a primary treatment method. Dry powder inhalers (DPIs) often face challenges related to particle aggregation, which can diminish drug delivery efficiency. This study investigates particle aggregation and aims to optimize the cohesion-adhesion balance to improve inhalation efficiency. Advanced techniques like atomic force microscopy and Raman imaging were used to analyze particle interactions, focusing on lactose ratios, particle morphology, and drug-drug interactions. The therapeutic efficacy of optimized formulations containing budesonide (BUD) and Arformoterol (AFT) was assessed using an asthma model, showing significant improvements in sRAW, neutrophil count, and tidal volume compared to the positive control, with <i>p</i>-values below 0.01. AFT exhibited comparable efficacy to Formoterol at half the dose. Additionally, pharmacokinetic studies demonstrated similar in vivo behavior between the drugs, confirming the therapeutic advantage of AFT, with <i>p</i>-values for AUC<sub>0-t</sub> and Cmax of .646 and .153, respectively. The fine particle fractions for AFT and BUD were 39.4% and 50.6%, respectively, indicating improved drug delivery efficiency and potential for better clinical outcomes in asthma and COPD patients.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"966-975"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472336","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Studies on allantoin topical formulations: in vitro drug release studies and rheological characteristics.","authors":"Alisa Elezović, Amar Elezović, Miroslav Hadnađev, Adna Džemat, Emina Hrnčić, Belma Imamović, Ervina Bečić, Veljko Krstonošić","doi":"10.1080/10837450.2024.2414938","DOIUrl":"10.1080/10837450.2024.2414938","url":null,"abstract":"<p><p>The extent and rate of release of active substances from topical products must be sufficient to ensure their effectiveness, which depends on selecting the most appropriate formulation. This study examined allantoin emulsions and gel formulations. In water-in-oil (W/O) and oil-in-water (O/W) emulsions, the main emulsifier was varied, while the same gelling agent was used in all formulations to test the effects of oil phase presence and emulsifier type on allantoin release, as well as the formulations' rheological and textural characteristics. O/W emulsions exhibited similar release rates and the overall amount released over six hours (11-14.8%), while the highest amount of allantoin (20.9%) was released from the gel formulation. Conversely, the amount of allantoin released from the W/O emulsion (0.77%) was insufficient. Experimental data generally fit best with the Higuchi model kinetics. The formulations demonstrated shear-thinning thixotropic behavior. The greatest deviation from the Newtonian type of flow, with the smallest value of constant n (0.106-0.13) and the largest thixotropic loop area (6602.67-8140 Pas<sup>-1</sup>) were shown by O/W emulsions. The W/O emulsion exhibited the highest constant n (0.70) and smaller hysteresis area (991.23 Pas<sup>-1</sup>). Firmness and consistency values increased in the order: gel < W/O emulsion < O/W emulsions. The O/W emulsions showed similarity in microstructure and textural characteristics, likely explaining their similar release behavior.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1033-1041"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472339","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Challenges and recent advances in erythropoietin stability.","authors":"Bahgat Fayed, Shanshan Luo, Alaa Eldeen B Yassin","doi":"10.1080/10837450.2024.2410448","DOIUrl":"10.1080/10837450.2024.2410448","url":null,"abstract":"<p><p>Erythropoietin (EPO) is a pivotal hormone that regulates red blood cell production, predominantly synthesized by the kidneys and also produced by the liver. Since the introduction of recombinant human EPO (rh-EPO) in 1989 through recombinant DNA technology, the therapeutic landscape for anemia has been improved. rh-EPO's market expansion has been substantial, with its application extending across various conditions such as chronic kidney disease, cancer-related anemia, and other disorders. Despite its success, significant concerns remain regarding the stability of EPO, which is critical for preserving its biological activity and ensuring therapeutic efficacy under diverse environmental conditions. Instability issues, including degradation and loss of biological activity, challenge both drug development and treatment outcomes. Factors contributing to EPO instability include temperature fluctuations, light exposure, and interactions with other substances. To overcome these challenges, pharmaceutical research has focused on developing innovative strategies such as stabilizing agents, advanced formulation techniques, and optimized storage conditions. This review article explores the multifaceted aspects of EPO stability, examining the impact of instability on clinical efficacy and drug development. It also provides a comprehensive review of current stabilization strategies, including the use of excipients, lyophilization, and novel delivery systems.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"930-944"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351886","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Vijayakumari Mahadevan Hari Priya, Anand Ganapathy A, Midhu George Veeran, Shyni Raphael M, Alaganandam Kumaran
{"title":"Nanotechnology-based drug delivery platforms for erectile dysfunction: addressing efficacy, safety, and bioavailability concerns.","authors":"Vijayakumari Mahadevan Hari Priya, Anand Ganapathy A, Midhu George Veeran, Shyni Raphael M, Alaganandam Kumaran","doi":"10.1080/10837450.2024.2414379","DOIUrl":"10.1080/10837450.2024.2414379","url":null,"abstract":"<p><p>Erectile dysfunction (ED), is a common and multidimensional sexual disorder, which comprises changes among any of the processes of the erectile response such as organic, relational, and psychological. However, both endocrine and nonendocrine causes of ED produce substantial health implications including depression and anxiety due to poor sexual performance, eventually affecting man's life eminence. Marginally invasive interventions following ED consist of lifestyle modifications, oral drugs, injections, vacuum erection devices, etc. Nevertheless, these conventional treatment regimens follow certain drawbacks such as efficacy and safety issues, and navigate to the development of novel therapeutic approaches such as nanomedicine for ED management. Nanotechnology-centred drug delivery platforms are being explored to minimize these limitations with better <i>in vitro</i> and <i>in vivo</i> effectiveness. Moreover, nanomedicine and nanocarrier-linked approaches are rapidly developing science in the nanoscale range, which contributes to site-specific delivery in a controlled manner and has generated considerable interest prominent to their potential to enhance bioavailability, decrease side effects, and avoidance of first-pass metabolism. This review provides an overview of recent discoveries regarding various nanocarriers and nano-delivery methods, along with current trends in the clinical aspects of ED. Additionally, strategies for clinical translation have been incorporated.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"996-1015"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142400977","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Serdar Tort, Ziya Canberk Öztürk, Fatma Kaynak-Onurdağ, N Başaran Mutlu-Ağardan
{"title":"Preparation and evaluation the effects of retinoic acid loaded proliposomal nanofibers on microbial biofilm inhibition.","authors":"Serdar Tort, Ziya Canberk Öztürk, Fatma Kaynak-Onurdağ, N Başaran Mutlu-Ağardan","doi":"10.1080/10837450.2024.2411034","DOIUrl":"10.1080/10837450.2024.2411034","url":null,"abstract":"<p><p>The electrospinning method involves the production of different drug delivery systems using various polymers. The production of proliposomes with electrospinning provides the hybridization of two novel drug delivery systems. Retinoic acid, also known as all-trans retinoic acid (ATRA), is a common and effective drug for acne therapy. This study aimed to prepare ATRA-loaded proliposomal nanofibers and evaluate their effectiveness on microbial biofilm inhibition. Blank and ATRA-loaded proliposomal nanofiber formulations were fabricated in various polyvinylpyrrolidone, phosphatidylcholine and cholesterol ratios. TEM images verified the rapid formation of the liposomes after the hydration of nanofibers. The vesicle size, polydispersity index and zeta potential values of self-assembled liposomes were measured. The vesicle size values were found to be 321.9-363.8 nm with PDI values varying between 0.332 and 0.511 and zeta potential values of (-16.8) to (-20.5)mV. ATRA-loaded proliposomal nanofibers provided higher bioadhesion (0.25 mJ/cm<sup>2</sup>) than the commercial cream (0.07 mJ/cm<sup>2</sup>). The short-term stability results showed that the initial characteristics remained for three months at 4 °C. The proposed ATRA-loaded self-assembled proliposomal system provided antibacterial, fungistatic or fungicidal effects superior to retinoic acid itself and inhibited biofilm formation in lower concentrations. This approach can combine the stability advantage of nanofibers in the dry state with the high effectiveness of liposomes in acne treatment presenting antibacterial and anti-biofilm-forming activity against <i>Candida albicans</i> and <i>Cutibacterium acnes</i>.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"955-965"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351888","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"ROS-responsive glycol chitosan-linked prodrug nanoparticle as a nanoplatform for tumor chemo-photodynamic therapy.","authors":"Jingmou Yu, Mengqi Liu, Chao Zhang, Lizhen Cheng, Changchun Peng, Dengzhao Jiang, Wenbo Liu, Hongguang Jin, Jin Ren","doi":"10.1080/10837450.2024.2411027","DOIUrl":"10.1080/10837450.2024.2411027","url":null,"abstract":"<p><p>Herein, we designed and synthesized novel reactive oxygen species (ROS)-responsive glycol chitosan-doxorubicin (DOX) prodrug <i>via</i> a ROS-cleavable thioketal (TK) linker. The obtained GC-TK-DOX formed self-assembled nanoparticles of 312 nm in aqueous media. Photosensitizers zinc phthalocyanine (ZnPc)-loaded GC-TK-DOX (GC-TK-DOX/ZnPc) nanoparticles were fabricated by using a dialysis approach. The GC-TK-DOX and GC-TK-DOX/ZnPc nanoparticles were nearly spherical by transmission electron microscopy (TEM) observation. Under 660-nm laser irradiation, GC-TK-DOX/ZnPc could generate singlet oxygen. Further, GC-TK-DOX/ZnPc nanoparticles exhibited ROS-sensitive release of DOX and ZnPc <i>in vitro</i>. GC-TK-DOX/ZnPc with laser irradiation showed more drug uptake and higher cytotoxic effects than GC-TK-DOX/ZnPc without irradiation, free DOX and GC-TK-DOX in HeLa tumor cells. Overall, these findings suggested that GC-TK-DOX/ZnPc could be a promising nanoarchitecture for synergetic chemo-photodynamic therapy against tumors.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"945-954"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351890","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Facile fabrication of degradable, serrated polyethylene diacrylate microneedles using stereolithography.","authors":"Vedant Joshi, Nidhi Singh, Pallab Datta","doi":"10.1080/10837450.2024.2413146","DOIUrl":"10.1080/10837450.2024.2413146","url":null,"abstract":"<p><p>Microneedles have the potential for minimally invasive drug delivery. However, they are constrained by absence of rapid, scalable fabrication methods to produce intricate arrays and serrations for enhanced adhesion. 3D printing techniques like stereolithography (SLA) are fast, scalable modalities but SLAs require non-degradable and stiff resins. This work attempts to overcome this limitation by utilizing a poly (ethylene glycol diacrylate) (PEGDA, F3) resin and demonstrating its compatibility with a commercial SLA printer. FESEM images showed high printing efficiency of customized bioinks (F3) similar to commercial resins using SLA 3D printer. Mechanical endurance tests of whole MNA showed that MNs array printed from F3 resin (485 ± 5.73 N) required considerably less force than commercial F1 resin (880 ± 32.4 N). Penetration performance of F1 and F3 was found to be 10.8 ± 2.06 N and 0.705 ± 0.03 N. In-vitro degradation study in PBS showed that MNs fabricated from F3 resin exhibited degradation after 7 days, which was not observed with the commercial F1 resin provided by the manufacturer. The histology of porcine skin exhibited formation of triangular pores with pore length of 548 μm and efficient penetration into the deeper dermal layer. In conclusion, PEGDA can be used as for fabricating degradable, serrated solid MNs over commercial resin.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"976-986"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372522","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Eman A Bseiso, Nermin M Sheta, Khaled M Abdel-Haleem
{"title":"Recent progress in nanoparticulate-based intranasal delivery for treating of different central nervous system diseases.","authors":"Eman A Bseiso, Nermin M Sheta, Khaled M Abdel-Haleem","doi":"10.1080/10837450.2024.2409807","DOIUrl":"10.1080/10837450.2024.2409807","url":null,"abstract":"<p><p>Drug administration to the central nervous system (CNS) has become a great obstacle because of several biological barriers, such as the blood-brain barrier, therefore, brain targeting insights are a light for scientists to move forward for treating neurogenerative diseases using advanced non-invasive methods. The current demand is to use a potential direct route as the nasal administration to transport drugs into the brain enhancing the BBB permeability and hence, increasing the bioavailability. Interestingly, recent techniques have been implanted in formulating nanocarriers-based therapeutics for targeting and treating ischemic stroke using lipid or polymeric-based materials. Nanoparticulate delivery systems are set as an effective platform for brain targeting as polymeric nanoparticles and polymeric micelles or nanocarriers based on lipids for preventing drug efflux to promote optimal therapeutic medication concentration in the brain-diseased site. In recent years, there has been a notable increase in research publications and ongoing investigations on the utilization of drug-loading nanocarriers for the treatment of diverse CNS diseases. This review comprehensively depicts these dangerous neurological disorders, drug targeting challenges to CNS, and potential contributions as novel intranasal nano-formulations are being used to treat and regulate a variety of neurological diseases.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"913-929"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}